2135 Systemic pharmacokinetics and carbonic anhydrase inhibition of dorzolamide

2135 Systemic pharmacokinetics and carbonic anhydrase inhibition of dorzolamide

fir-pose: Dorzolamide @ORE) is a topical carbonic anhydrase (CA) inhibitor that is approved for treatment of open-angle glauccma and ocular hypertension. DORE exerts its effects directly in the eye at substantially lower doses and therefore with less systemic exposure than oral CA inhibitors To evaluate DORZ's potential for systemic CA inhibition, maximum systemic exposure was simulated through...

Carbonic anhydrase: chemistry, physiology, and inhibition.

Non-Classical Inhibition of Carbonic Anhydrase

Specific isoforms from the carbonic anhydrase (CA) family of zinc metalloenzymes have been associated with a variety of diseases. Isoform-specific carbonic anhydrase inhibitors (CAIs) are therefore a major focus of attention for specific disease treatments. Classical CAIs, primarily sulfonamide-based compounds and their bioisosteres, are examined as antiglaucoma, antiepileptic, antiobesity, ant...

Toxic Epidermal Necrolysis Induced by the Topical Carbonic Anhydrase Inhibitors Brinzolamide and Dorzolamide.

Brinzolamide and dorzolamide are highly specific topical carbonic anhydrase inhibitors (CAIs). They lower intraocular pressure (IOP) by reducing the rate of aqueous humour formation without serious side effects. Although systemic CAIs are the most potent medications for lowering intraocular pressure for conditions with ocular hypertension, many cases with adverse systemic reactions have been re...

Catalysis and inhibition of human carbonic anhydrase IV.

Carbonic anhydrase IV (CA IV) is a membrane-bound form of carbonic anhydrase. We have characterized the catalytic activity and inhibition of recombinant human CA IV. CA IV is a high-activity isozyme in CO2 hydration with a pH-independent kcat value (1.1 x 10(6) s(-1)) comparable to that of CA II (8 x 10(5) s(-1)). Furthermore, CA IV is more active in HCO3- dehydration than is CA II as illustrat...